2,3-disubstituted isoxazolidines, agents containing them and the

Details 2,3-disubstituted isoxazolidines, agents containing them and the 2,3-disubstituted isoxazolidines, agents containing them and the

1993-04-16

1995-06-06

Brust, Joseph Paul

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 19, 514378, 530331, 548240, A61K 3805, A61K 3806, C07D26102

Patent

active

054223423

ABSTRACT:
The invention relates to compounds of the formula ##STR1## in which A denotes an optionally substituted radical from the series comprising alkyl, acyl, cycloalkyl, aryl and heteroaryl; A.sub.1 represents CO, CS, C=NH, CN-alkyl, CN-O-alkyl, SO, optionally substituted CH.sub.2 or a bond; A.sub.2 represents NH, NCH.sub.3, O, CH.sub.2 or a bond; E represents CHOH, CO, SO or optionally N-substituted C=NH; A.sub.3 represents O, NH, NCH.sub.3 or a bond; R.sup.4 denotes an optionally substituted radical from the series comprising alkyl, cycloalkyl, aryl and heteroaryl; and R.sup.8 denotes hydrogen or optionally substituted alkyl, to a process for their preparation, and to their use as inhibitors of prolyl hydroxylase.

REFERENCES:
patent: 3944562 (1976-03-01), Martin et al.
patent: 4269772 (1981-05-01), Melillo et al.
patent: 4457936 (1984-07-01), Draeger et al.
patent: 4562187 (1985-12-01), Tegeler et al.
V. Gunzler et al, The Journal of Biological Chemistry, vol. 263, No. 36, pp. 19498-19504, 1988.
A. Vessella et al., Chemical Abstracts, vol. 95, No. 7, p. 706, 95:62045p (1981).
A. Vessella et al., Chemical Abstracts, vol. 99, No. 19, p. 654 99:158804u (1983).

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